Polycyclo Ring System Having The Additional Hetero Ring As One Of The Cyclos Patents (Class 514/232.8)
  • Patent number: 10322128
    Abstract: The present invention provides compositions and methods for the treatment of neoplasms, in particular, by targeting of quiescent cancer cells with therapeutic agents in combination with other treatments effective against certain neoplastic conditions, in particular, anti-cancer treatment with EGFR inhibitor agents.
    Type: Grant
    Filed: April 14, 2017
    Date of Patent: June 18, 2019
    Assignee: Felicitex Therapeutics, Inc.
    Inventors: Maria Vilenchik, Michael Frid, Alexandra Kuznetsova, Yuriy Gankin, Marc Duey
  • Patent number: 10314843
    Abstract: The present invention provides compositions and methods for the treatment of neoplasms, in particular, by targeting of quiescent cancer cells with therapeutic agents in combination with other treatments effective against certain neoplastic conditions, in particular, anti-cancer treatment with therapeutic agents that are inhibitors of mitosis (a mitotic inhibitor).
    Type: Grant
    Filed: April 14, 2017
    Date of Patent: June 11, 2019
    Assignee: Felicitex Therapeutics, Inc.
    Inventors: Maria Vilenchik, Michael Frid, Alexandra Kuznetsova, Yuriy Gankin, Marc Duey
  • Patent number: 10106552
    Abstract: Eukaryotic elongation factor 2 kinase inhibitors of the formula where R1, R2, R3a, R3b, R4a, R4b, R5a, R5b, R6a, R6b, R7 and x are as defined in the specification, pharmaceutical compositions and formulations including compounds of the foregoing formula, and methods of preventing, ameliorating or treating indications, conditions, disorders or syndromes associated with elongation factor 2 phosphorylation.
    Type: Grant
    Filed: May 12, 2016
    Date of Patent: October 23, 2018
    Assignee: Longevica Pharmaceuticals, Inc.
    Inventor: John H. Dodd
  • Patent number: 9951061
    Abstract: The present invention provides compounds useful as inhibitors of Ca2+/calmodulin-dependent protein kinase (CaMKII), compositions thereof, and methods of using the same.
    Type: Grant
    Filed: March 5, 2014
    Date of Patent: April 24, 2018
    Assignee: Allosteros Therapeutics, Inc.
    Inventors: Daniel E. Levy, Howard Schulman, Bheema Paraselli, Erin Bradley, Sampath K. Nangunoori, Brahmaiah Dabbugoddu, Isabelle Lehoux
  • Patent number: 9783539
    Abstract: Disclosed herein are certain indoloquinolone compounds, methods of preparation thereof, pharmaceutical compositions thereof, and uses thereof, such as their uses as ALK inhibitors.
    Type: Grant
    Filed: February 27, 2014
    Date of Patent: October 10, 2017
    Assignee: Jiangsu Ascentage Biomed Development Inc.
    Inventors: Jianyong Chen, Yunlong Zhou, Shaomeng Wang, Ming Guo, Dajun Yang, Lingling Jiao, Yu Jing, Xu Qian, Liu Liu, Longchuan Bai, Chao-Yie Yang, Donna McEachern
  • Patent number: 9745314
    Abstract: Inhibitors of MDM2 and MDM2-related proteins and compositions containing the same are disclosed. Methods of using the MDM2 inhibitors in the treatment of diseases and conditions wherein inhibition of an interaction between p53 and MDM2 provides a benefit, like cancers, also are disclosed.
    Type: Grant
    Filed: April 16, 2015
    Date of Patent: August 29, 2017
    Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Shaomeng Wang, Angelo Aguilar, Liu Liu, Jianfeng Lu, Donna McEachern
  • Patent number: 9624238
    Abstract: Compounds that may be used to inhibit Notum Pectinacetylesterase are described, as well as compositions comprising them, and methods of their use to treat diseases and disorders affecting bone.
    Type: Grant
    Filed: May 21, 2014
    Date of Patent: April 18, 2017
    Assignee: Lexicon Pharmaceuticals, Inc.
    Inventors: Joseph Barbosa, Kenneth Gordon Carson, Michael Walter Gardyan, Jason Patrick Healy, Qiang Han, Ross Mabon, Praveen Pabba, James Tarver, Jr., Kristen M. Terranova, Ashok Tunoori, Xiaolian Xu
  • Patent number: 9493460
    Abstract: The invention relates to novel compounds which are naphthalene diimides of general formula (I): The compounds are used in therapy, particularly in cancer treatment.
    Type: Grant
    Filed: March 13, 2013
    Date of Patent: November 15, 2016
    Assignee: UCL BUSINESS PLC
    Inventors: Stephen Neidle, Stephan A. Ohnmacht, Mekala Gunaratnam, Aaron Grainger Dale, Marialuisa Micco, Gavin William Collie
  • Patent number: 9388250
    Abstract: Soluble adenylyl cyclase (sAC) is implicated in proliferation of keratinocytes. Inhibitors of sAC are useful for the treatment and/or prevention of psoriasis and other hyperproliferative skin disorders. Assays to identify such compounds are also described.
    Type: Grant
    Filed: February 23, 2010
    Date of Patent: July 12, 2016
    Assignee: CORNELL UNIVERSITY
    Inventors: Jochen Buck, Lonny Levin, Jonathan Zippin
  • Patent number: 9365489
    Abstract: The present invention relates to a method for reducing the production of methane emanating from the digestive activities of a ruminant and or for improving ruminant animal performance by using, as active compound at least one nitrooxy alkanoic acid and/or derivative thereof, which is administrated to the animal together with the feed. The invention also relates to the use of these compounds in feed and feed additives such as premix, concentrates and total mixed ration (TMR) or in the form of a bolus.
    Type: Grant
    Filed: January 21, 2014
    Date of Patent: June 14, 2016
    Assignee: DSM IP ASSETS B.V.
    Inventors: Stephane Duval, Maik Kindermann
  • Patent number: 9334288
    Abstract: Compounds, compositions and methods are provided that comprise selective ?-glucuronidase inhibitors for both aerobic and anaerobic bacteria, especially enteric bacteria normally associated with the gastrointestinal tract. The compounds, compositions and methods can be for inhibiting bacterial ?-glucuronidase and for improving efficacy of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds by attenuating the side effects caused by reactivation by bacterial ?-glucuronidases of glucuronidated metabolites of camptothecin-derived antineoplasatic agents or glucuronidase-substrate agents or compounds.
    Type: Grant
    Filed: September 23, 2013
    Date of Patent: May 10, 2016
    Assignee: The University of North Carolina at Chapel Hill
    Inventor: Matthew R. Redinbo
  • Patent number: 9315458
    Abstract: The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity and useful as an agent for the prophylaxis or treatment of Alzheimer's disease, schizophrenia, pain, sleep disorder, Parkinson's disease dementia, dementia with Lewy bodies, and the like. The present invention relates to a compound represented by the formula (I) or a salt thereof. wherein each symbol is as described in the specification, or a salt thereof.
    Type: Grant
    Filed: April 22, 2015
    Date of Patent: April 19, 2016
    Assignee: Takeda Pharmaceutical Company, Limited
    Inventors: Masami Yamada, Shinkichi Suzuki, Takahiro Sugimoto, Minoru Nakamura, Hiroki Sakamoto, Makoto Kamata
  • Patent number: 9283244
    Abstract: Inhibitors of Late SV-40 Factor (LSF) are used to treat cancers such as hepatocellular carcinoma (HCC). In particular, small molecule chemical LSF inhibitors are employed. In addition, the activity and/or pattern of expression of LSF may is used to diagnose cancer, to characterize the cancer (e.g. stage, grade, prognosis, etc.) and also to develop suitable protocols for cancer treatment.
    Type: Grant
    Filed: March 29, 2011
    Date of Patent: March 15, 2016
    Assignee: Virginia Commonwealth University
    Inventors: Devanand Sarkar, Paul B. Fisher
  • Patent number: 9284332
    Abstract: Provided herein are process for the preparation of N-(5-ferf-butyl-isoxazol-3-yl)-N?-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-fe][1,3]benzothiazol-2-yl]phenyl}urea, or a pharmaceutically acceptable salt, solvate, hydrate, or polymorph thereof. N-(5-tert-Butyl-isoxazol-3-yl)-N?-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-&][1,3]benzo-thiazol-2-yl]phenyl}urea is useful for treating, preventing, and/or managing diseases or conditions, including but not limited to, proliferative diseases, FLT-3 mediated diseases, and cancers.
    Type: Grant
    Filed: November 4, 2010
    Date of Patent: March 15, 2016
    Assignee: Ambit Biosciences Corporation
    Inventors: Timothy David Gross, Rathan Prasad Achampeta, Janakiram Rao Citineni
  • Patent number: 9238656
    Abstract: This application relates to compounds of the Formula I as defined herein, and/or salts thereof. This application further relates to compositions and methods of using these compounds and/or salts thereof. The compounds of Formula I are useful as ALK and JAK modulators for the treatment of proliferative disorders.
    Type: Grant
    Filed: July 30, 2014
    Date of Patent: January 19, 2016
    Assignee: Cephalon, Inc.
    Inventors: Henry J. Breslin, Matthew A. Curry, Diane E. Gingrich, Keith S. Learn, Gregory R. Ott, Jason C. Wagner
  • Patent number: 9238571
    Abstract: The instant invention relates to pharmaceutical compositions containing c-Met kinase inhibitors. Also disclosed are processes for making said pharmaceutical compositions.
    Type: Grant
    Filed: September 21, 2010
    Date of Patent: January 19, 2016
    Assignee: Merck Sharp & Dohme Limited
    Inventor: Robert Ward
  • Patent number: 9206200
    Abstract: The present invention is directed to N-linked lactam compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Grant
    Filed: May 11, 2012
    Date of Patent: December 8, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Kuduk, Douglas C. Beshore, Zhi-Qiang Yang, Youheng Shu, Daniel Pitts
  • Patent number: 9198915
    Abstract: Embodiments of the invention include methods and compositions involving aldose reductase inhibitors for the treatment of inflammation, including uveitis and asthma.
    Type: Grant
    Filed: September 17, 2012
    Date of Patent: December 1, 2015
    Assignee: The Board of Regents of the University of Texas System
    Inventors: Satish K. Srivastava, Kota V. Ramana
  • Patent number: 9155797
    Abstract: The invention relates to (among other things) oligomer-cannabinoid conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over previously administered un-conjugated cannabinoid compounds.
    Type: Grant
    Filed: July 22, 2014
    Date of Patent: October 13, 2015
    Assignee: Nektar Therapeutics
    Inventors: Jennifer Riggs-Sauthier, C. Simone Jude-Fishburn, Guy Lalonde
  • Patent number: 9115133
    Abstract: The present invention relates to substituted fused tricyclic compounds of formula (I) or (Ia), their tautomers, polymorphs, stereoisomers, prodrugs, solvates, co-crystals, pharmaceutically acceptable salts, pharmaceutical compositions containing them and methods of treating conditions and diseases that are mediated by JAK activity. The compounds of the present invention are useful in the treatment, prevention or suppression of diseases and disorders mediated by JAK activity.
    Type: Grant
    Filed: March 21, 2012
    Date of Patent: August 25, 2015
    Assignee: Advinus Therapeutics Limited
    Inventors: Dinesh Barawkar, Tanushree Bende, Robert Zahler, Anish Bandyopadhyay, Robindro Singh Sarangthem, Jignesh Doshi, Yogesh Waman, Rushikesh Jadhav, Umesh Prasad Singh
  • Publication number: 20150148318
    Abstract: A method of inhibiting the growth of cancer cells is disclosed in which cancer cells that contain an enhanced amount relative to non-cancerous cells of one or more of phosphorylated mTOR, Akt1, ERK2 and serine2152-phosphorylated filamin A are contacted with an FLNA-binding effective amount of a compound or a pharmaceutically acceptable salt thereof that binds to the pentapeptide of filamin A (FLNA) of SEQ ID NO: 1 and exhibits at least about 60 percent of the FITC-labeled naloxone binding amount when present at a 10 ?M concentration and using unlabeled naloxone as the control inhibitor at the same concentration. A compound that binds to the FLNA pentapeptide preferably also contains at least four of the six pharmacophores of FIGS. 19-24.
    Type: Application
    Filed: September 26, 2014
    Publication date: May 28, 2015
    Inventors: Hoau-Yan Wang, Lindsay Burns Barbier
  • Publication number: 20150148314
    Abstract: There are provided, inter alia, derivatives of seriniquinone and methods useful for the treatment of cancer, and in particular treatment of melanoma and prostate cancer.
    Type: Application
    Filed: January 27, 2015
    Publication date: May 28, 2015
    Inventors: William Fenical, Paul R. Jensen, James J. La Clair, Lynnie Trzoss, Takashi Fukuda
  • Patent number: 9040528
    Abstract: The present invention relates to compounds of Formula (I): to pharmaceutically acceptable salts thereof, to methods of using them to treat bacterial infections, and to methods for their preparation.
    Type: Grant
    Filed: January 13, 2014
    Date of Patent: May 26, 2015
    Assignee: AstraZeneca AB
    Inventors: Kevin Barvian, Gregory Steven Basarab, Madhusudhan Reddy Gowravaram, Sheila Irene Hauck, Fei Zhou
  • Publication number: 20150141418
    Abstract: The present invention relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for inhibiting VEGF production.
    Type: Application
    Filed: January 26, 2015
    Publication date: May 21, 2015
    Applicant: PTC Therapeutics, Inc.
    Inventors: William Lennox, Hongyan Qi, Duck-Hyung Lee, Soongyu Choi, Young-Choon Moon
  • Patent number: 9034870
    Abstract: The invention described herein pertains to substituted azaindenoisoquinoline compounds, in particular 7-, 8-, 9-, and 10-azaindenoisoquinoline compounds, which are inhibitors of topoisomerase I, processes and intermediates for their syntheses, pharmaceutical compositions of the compounds, and methods of using them in the treatment of cancer.
    Type: Grant
    Filed: March 6, 2014
    Date of Patent: May 19, 2015
    Assignees: Purdue Research Foundation, United States Government National Institutes of Health (NIH), U.S. Dept. of Health and Human Services (DHHS), NIH Division of Extramural Inventions and Technology Resources (DEITR)
    Inventors: Mark S. Cushman, Evgeny A. Kiselev, Andrew E. Morrell, Yves George Pommier
  • Publication number: 20150133443
    Abstract: The present invention relates to substituted thiazolyl- and oxazolyl-isoquinolinones that act, for example, as modulators of poly(ADP-ribose) polymerase (PARP). The present invention also relates to processes for the preparation of substituted thiazolyl- and oxazolyl-isoquinolinones and to their use in treating various diseases and disorders.
    Type: Application
    Filed: November 7, 2014
    Publication date: May 14, 2015
    Inventors: Roberto Pellicciari, Flavio Moroni
  • Publication number: 20150133445
    Abstract: The invention described herein pertains to the synthesis and use of certain N-substituted indenoisoquinoline compounds which inhibit the activity Tyrosyl-DNA Phosphodiesterase I (Tdp1) or Topoisomerase I (Top1) or both, or otherwise demonstrate anticancer activity. Also disclosed are novel N-substituted indenoisoquinoline compounds and pharmaceutical compositions comprising the novel N-substituted indenoisoquinoline compounds.
    Type: Application
    Filed: November 10, 2014
    Publication date: May 14, 2015
    Inventors: Mark S. CUSHMAN, Trung X. Nguyen, Martin M. Conda-Sheridan, Yves George Pommier
  • Publication number: 20150133442
    Abstract: The invention features compositions and methods for inhibiting the Pin1 protein, and the treatment of disorders characterized by elevated Pin1 levels.
    Type: Application
    Filed: June 7, 2013
    Publication date: May 14, 2015
    Inventors: Kun Ping Lu, Matthew Brian Boxer, Mindy Irene Emily Davis, Rajan Pragani, Min Shen, Anton Momtchilov Simeonov, Shuo Wei, Xiao Zhen Zhou
  • Publication number: 20150132352
    Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present invention provides compounds as therapeutic agents against bacterial infections (e.g., biofilms).
    Type: Application
    Filed: May 2, 2013
    Publication date: May 14, 2015
    Inventors: Hongmin Sun, Bryan Yestrepsky, David Ginsburg, Scott D. Larsen
  • Publication number: 20150133425
    Abstract: The present invention relates to substituted thienopyrimidine compounds of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: May 17, 2013
    Publication date: May 14, 2015
    Inventors: Georg Kettschau, Florian Puehler, Knut Eis, Ulrich Klar, Dirk Kosemund, Detlev Sülzle, Philip Lienau, Andrea Hägebarth, Ulf Bömer, Lars Wortmann, Keith Graham, Antje Margret Wengner
  • Publication number: 20150133426
    Abstract: The present invention relates to substituted pyrrolopyrimidine compounds general formula I: in which A, X, R1, R2, m and n are as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: May 17, 2013
    Publication date: May 14, 2015
    Inventors: Ulrich Klar, Georg Kettschau, Detlev Sülzle, Florian Puehler, Dirk Kosemund, Philip Lienau, Ulf Bömer, Lars Wortmann
  • Publication number: 20150133444
    Abstract: The present disclosure provides derivatives of melampomagnolide B (MMB), including carbonates, carbamates, and thiocarbamates. The derivatives may be synthesized via an MMB triazole intermediate. These derivatives are useful for treating cancer in humans.
    Type: Application
    Filed: November 10, 2014
    Publication date: May 14, 2015
    Inventors: Venumadhav Janganati, Narsimha Reddy Penthala, Peter A. Crooks, Craig T. Jordan
  • Patent number: 9029387
    Abstract: The present invention relates to benzonaphthyridinamines of the formula (I) as autotaxin inhibitors and to the use thereof in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions in which the inhibition, regulation and/or modulation of phosphodiesterase or lysophospholipase autotaxin plays a role, in particular of various types of cancer and autoimmune and inflammatory diseases.
    Type: Grant
    Filed: February 28, 2011
    Date of Patent: May 12, 2015
    Assignee: Merck Patent GmbH
    Inventors: Wolfgang Staehle, Melanie Schultz, Kai Schiemann
  • Publication number: 20150126491
    Abstract: Compounds of the formula I: or a pharmaceutical salt thereof, wherein X, Ar1, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Application
    Filed: November 5, 2014
    Publication date: May 7, 2015
    Applicant: Genentech, Inc.
    Inventors: Monique Bodil van Niel, Andrew Cridland, Benjamin Fauber, Alberto Gobbi, Christopher Hurley, David Hurst, Jonathan Killen, Robert Maxey, Stuart Ward
  • Publication number: 20150126501
    Abstract: The present invention belongs to the technical field of medicine, relating in particular to: a fused ring compound as represented by Formula (I) for use as a mineralocorticoid receptor antagonist, a pharmaceutically acceptable salt thereof, and an isomer thereof; a preparation method for these compounds; a pharmaceutical preparation containing these compounds; and an application of these compounds, the pharmaceutically acceptable salt thereof, or the isomers thereof in the preparation of medicants for the treatment and/or prevention of kidney injury, cardiovascular diseases such as hypertension, and/or endocrine disease. The definitions of X, Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4, Cy and n are as presented in the description.
    Type: Application
    Filed: January 7, 2015
    Publication date: May 7, 2015
    Inventors: Zhenhua Huang, Jinyuan Wang, Dedong Zhang
  • Publication number: 20150119388
    Abstract: An ester of ArOH according to the formula R—X—CO—OAr, wherein ArOH is a pharmaceutically active compound selected from the group consisting of SN-38, PI-103, etoposide and fenretinide, wherein a) R is a residue of cholesterol, sitosterol, SN-38, PI-103, etoposide or fenretinide and X is O—CO-L, wherein L is either a direct bond or a linking group including a branched or unbranched hydrocarbyl moiety that may optionally include in-chain or pendant heteroatom substituents and/or cyclic moieties; b) R—X—CO-0 is an all-trans retinoate radical or the 9-cis or 13-cis isomer thereof; or c) R—X— is a branched or unbranched, saturated or unsaturated hydrocarbyl moiety comprising at least 5 carbon atoms and optionally including at least one in-chain or pendant heteroatom substituent and/or cyclic moiety.
    Type: Application
    Filed: June 14, 2013
    Publication date: April 30, 2015
    Applicant: THE CHILDREN'S HOSPITAL PHILADELPHIA
    Inventors: Ivan Alferiev, Michael Chorny, Garrett M. Brodeur, Robert J. Levy
  • Publication number: 20150119389
    Abstract: Compounds of the formula Ia***** in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors, useful in the treatment of psoriasis.
    Type: Application
    Filed: October 7, 2014
    Publication date: April 30, 2015
    Inventor: Ulrich KAUTZ
  • Patent number: 9018201
    Abstract: A compound having the structure set forth in Formula (I) and Formula (II): wherein the substituents Y, Z, A, B, R1, R2, R3, R4 and R5 are as defined herein. Provided herein are inhibitors of poly(ADP-ribose)polymerase activity. Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat diseases, disorders and conditions associated with a PTEN deficiency that are ameliorated by the inhibition of PARP activity.
    Type: Grant
    Filed: August 21, 2013
    Date of Patent: April 28, 2015
    Assignee: Biomarin Pharmaceuticial Inc.
    Inventors: Daniel Chu, Bing Wang, Ying Feng, Yuqiao Shen, Leonard Edwin Post
  • Patent number: 9006234
    Abstract: This disclosure relates to new compounds that may be used to modulate a histamine receptor in an individual. Novel compounds are described, including new bridged heterocyclic[4,3-b]indole compounds. Pharmaceutical compositions are also provided. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Grant
    Filed: July 2, 2012
    Date of Patent: April 14, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: Rajendra Parasmal Jain, Sarvajit Chakravarty
  • Publication number: 20150099731
    Abstract: The present invention provides compounds of the formula (I) wherein: X1, X2 and X3 are heteroatoms; R4, R5, R6, R7, R8, R9 and R10 are independently selected from H, halo, —OH, —NO2, —CN and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; and Z is optionally substituted C1-8 straight-chained or branched aliphatic, optionally containing 1 or more double or triple bonds, wherein one or more carbons are optionally replaced by R* wherein R* is optionally substituted cycloalkyl, heterocycloalkyl, aryl or heteroaryl; an amino acid residue, H, —CN, —C(O)—, —C(O)C(O)—, —C(O)NR1—, —C(O)NR1NR2—, —C(O)O—, —OC(O)—, —NR1CO2—, —O—, —NR1C(O)NR2—, —OC(O)NR1—, —NR1NR2—, —NR1C(O)—, —S—, —SO—, —SO2—, —NR1—, —SO2NR1—, —NR1R2, or —NR1SO2—, wherein R1 and R2 are independently selected from H and optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; or where R* is NR1R2, R1 and R2 optionally together with the nitrogen atom form an optionally substituted 5-12 me
    Type: Application
    Filed: May 5, 2014
    Publication date: April 9, 2015
    Applicant: University of Kentucky
    Inventors: Peter A. Crooks, Craig T. Jordan, Xiaochen Wei
  • Patent number: 8999978
    Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic [4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: April 7, 2015
    Assignee: Medivation Technologies, Inc.
    Inventors: David T. Hung, Andrew Asher Protter, Rajendra Parasmal Jain, Sundeep Dugar, Sarvajit Chakravarty
  • Publication number: 20150087630
    Abstract: Methods of use of compounds of formula (I) for treating cancer: wherein X, Y, X, R3, R5 and R6 are as defined herein.
    Type: Application
    Filed: April 17, 2014
    Publication date: March 26, 2015
    Applicant: Genentech, Inc.
    Inventors: Huifen Chen, Hazel Joan Dyke, Charles Ellwood, Emanuela Gancia, Lewis Gazzard, Simon Goodacre, Samuel Kintz, Joseph Lyssikatos, Calum MacLeod, Karen Williams
  • Publication number: 20150080389
    Abstract: The present invention provides heteroaryl ketone fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.
    Type: Application
    Filed: September 16, 2014
    Publication date: March 19, 2015
    Inventors: Hazel Hunt, Tony Johnson, Nicholas Ray, Iain Walters
  • Publication number: 20150079081
    Abstract: Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions. Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.
    Type: Application
    Filed: October 27, 2014
    Publication date: March 19, 2015
    Applicant: Genentech, Inc.
    Inventors: Jennafer Dotson, Robert Andrew Heald, Timothy Heffron, Graham Elgin Jones, Sussie Lerche Krintel, Neville James McLean, Chudi Ndubaku, Alan G. Olivero, Laurent Salphati, Lan Wang, BinQuing Wei
  • Publication number: 20150080390
    Abstract: The present invention relates generally to compositions and methods for treating diseases and disorders caused by herpes simplex virus type 1, including herpes simplex keratitis, in a subject. In certain embodiments, the compositions of the present invention comprise an ATM inhibitor and an anti-herpetic agent. In other embodiments, the compositions comprise a Chk2 inhibitor and an anti-herpetic agent. In yet other embodiments, the compositions comprise a Chk2 inhibitor and an ATM inhibitor, and optionally an anti-herpetic agent.
    Type: Application
    Filed: September 17, 2014
    Publication date: March 19, 2015
    Inventors: Jane E. Clifford, Oleg Alekseev, Stephen R. Jennings
  • Patent number: 8981131
    Abstract: The present invention provides compounds represented by formula I: wherein, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13 and X are as defined in the specification, in all its stereoisomeric and tautomeric forms and mixtures thereof in all ratios, and its pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable polymorphs and prodrugs. These compounds are useful for treatment of inflammatory disorders including those caused by elevated levels of proinflammatory cytokines such as Tumor Necrosis Factor (TNF-? and/or interleukins (IL-1?, IL-6, IL-8). The invention also relates to processes for the manufacture of compounds of formula 1 and pharmaceutical compositions containing them.
    Type: Grant
    Filed: July 25, 2008
    Date of Patent: March 17, 2015
    Assignee: Piramal Enterprises Limited
    Inventors: Dilip Narayanrao Bhedi, Ram Asrey Vishwakarma, Vaishali Deka, Dattatray Maruti More, Manivannan Ramalingam, Ashish Suthar, Roda Dalal, Sapna Parikh, Aditi Amol Tannu
  • Publication number: 20150065499
    Abstract: The present invention relates to compounds according to Formula I: and salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, X, and Y are as defined herein. Methods for preparing compounds of Formula I are also provided. The present invention further includes methods of treating cellular proliferative disorders, such as cancer, with the compounds of Formula I.
    Type: Application
    Filed: February 26, 2013
    Publication date: March 5, 2015
    Inventors: E. Premkumar Reddy, M. V. Ramana Reddy
  • Publication number: 20150065498
    Abstract: The present invention is directed to N-linked lactam compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Application
    Filed: May 11, 2012
    Publication date: March 5, 2015
    Inventors: Scott D. Kuduk, Douglas C. Beshore, Zhi-Qiang Yang, Youheng Shu, Daniel Pitts
  • Publication number: 20150051205
    Abstract: Compounds, compositions and methods are provided that comprise selective ?-glucuronidase inhibitors for both aerobic and anaerobic bacteria, especially enteric bacteria normally associated with the gastrointestinal tract. The compounds, compositions and methods can be for inhibiting bacterial ?-glucuronidase and for improving efficacy of camptothecin-derived antineoplastic agents or glucuronidase-substrate agents or compounds by attenuating the side effects caused by reactivation by bacterial ?-glucuronidases of glucuronidated metabolites of camptothecin-derived antineoplasatic agents or glucuronidase-substrate agents or compounds.
    Type: Application
    Filed: September 23, 2013
    Publication date: February 19, 2015
    Applicant: The University of North Carolina at Chapel Hill
    Inventor: Matthew R. Redinbo
  • Publication number: 20150051204
    Abstract: Present invention refers to new compounds of formula I or II, its synthesis and its use in the treatment of metabolic syndrome, particularly for the treatment of type I or type II diabetes and/or metabolic syndrome or metabolic disease or metabolic disorders.
    Type: Application
    Filed: March 28, 2012
    Publication date: February 19, 2015
    Applicant: SJT MOLECULAR RESEARCH, S.L.
    Inventors: Juan Carlos Agreda Navajas, Roberto Mikio Kassuya